Tirabrutinib

SKU: orb1679016

Description

Tirabrutinib (GS-4059/ONO-4059) is an orally bioavailable, covalent Bruton's Tyrosine Kinase (BTK) inhibitor (IC₅₀ = 6.8 nM) capable of crossing the blood-brain barrier. It suppresses aberrant B-cell receptor signaling and is utilized in research for B-cell malignancies like Waldenström's macroglobulinemia and autoimmune disorders, with applications in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1351636-18-4
• MW: 454.48
• Purity: 99.75% (May vary between batches)
• Formula: C₂₅H₂₂N₆O₃
• SMILES: CC#CC(=O)N1CC[C@H](C1)n1c2ncnc(N)c2n(-c2ccc(Oc3ccccc3)cc2)c1=O
• Target: BTK,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.26 mM);DMSO:90 mg/mL (198.03 mM)

Bioactivity

• Target IC50:
  ERBB2:7.31 μM|BLK:0.3 μM|JAK3:5.52 μM|BTK:2.2 nM|EGFR:3.02 μM|TEC:48 nM|TXK:92 nM|BMX kinase:6 nM|ERB4:0.77 μM
• In Vivo:
  Tirabrutinib (10 mg/kg; p.o.; single) is rapidly absorbed into plasma and brain, reaching Cmax (blood Cmax = 339.53 ng/mL; brain Cmax = 28.9 ng/mL) 2 hours post-administration. Additionally, Tirabrutinib (6, 20 mg/kg; p.o.; single daily for 3 weeks) inhibits tumor growth in vivo.
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• In Vitro:
  Tirabrutinib (0.1-1000 nM or 0.001-100 nM; 72 h) inhibits the proliferation of OCI-LY10 and SU-DHL-6 cells with IC50s of 9.127 nM and 17.10 nM, respectively. Tirabrutinib (0.5, 5, 50 μM; 24, 48 h) induces apoptosis in SU-DHL-6 cells, requiring high dosage and prolonged administration (up to 50 μM for 48 h). Tirabrutinib (300 nM, 72 h) induces caspase-3 and PARP cleavage in TMD8 cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tirabrutinib, Velexbru, ONO 4059, ONO4059, ONO-4059, GS4059, GS-4059, GS 4059, BTK

Compound Identifiers

PubChem CID

54755438